Patent SG-11201809162X-A (SG)
Title: 6-aminopyridin-3-yl thiazoles as modulators of ror?t
Inventor: MCCLURE KELLY
IPC: C07D498/08
Filed: 2017-04-26
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1#11101111 0 11101 HOE 010 1111 1 0 I 0111011101111111111 01111111011110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2017/189661 Al 02 November 2017 (02.11.2017) WIP0 I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07D 417/04 (2006.01) C07D 491/107 (2006.01) kind of national protection available): AE, AG, AL, AM, CO7D 491/08 (2006.01) CO7D 498/08 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CO7D 417/14 (2006.01) A61K 31/4439 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, CO7D 487/08 (2006.01) A61P 29/00 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (21) International Application Number: HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, PCT/US2017/029531 KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (22) International Filing Date: PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, 26 April 2017 (26.04.2017) SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 62/328,074 27 April 2016 (27.04.2016) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (71) Applicant: JANSSEN PHARMACEUTICA NV EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, [BE/BE]; Turnhoutseweg 30, B-2340 Beerse (BE). MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (72) Inventor; and TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (71) Applicant (for US only): GOLDBERG, Steven [US/US]; KM, ML, MR, NE, SN, TD, TG). _ 3210 Merryfield Row, San Diego, California 92121 (US). Declarations under Rule 4.17: = Inventors: MCCLURE, Kelly; 3210 Merryfield Row, San — as to applicant's entitlement to apply for and be granted a (72) Diego, California 92121 (US). TANIS, Virginia M.; 3210 patent (Rule 4.17(ii)) = Merryfield Row, San Diego, California 92121 (US). FEN- — as to the applicant's entitlement to claim the priority of the NEMA, Elizabeth G.; 3210 Merryfield Row, San Diego, earlier application (Rule 4.17(iii)) California 92121 (US). LEBSACK, Alec D.; 3210 Merry- field Row, San Diego, California 92121 (US). MARTIN, Published: Connor L.; 3210 Merryfield Row, San Diego, California — with international search report (Art. 21(3)) = — = 92121 (US). VENKATESAN, Hariharan; 3210 Merry- — before the expiration of the time limit for amending the field Row, San Diego, California 92121 (US). XUE, Xiao- claims and to be republished in the event of receipt of = — hua; 3210 Merryfield Row, San Diego, California 92121 amendments (Rule 48.2(h)) = (US). WOODS, Craig R.; 3210 Merryfield Row, San — with sequence listing part of description (Rule 5.2(a)) _ Diego, California 92121 (US). = Agent: SHIRTZ, Joseph F. et al.; Johnson & Johnson, (74) — = One Johnson & Johnson Plaza, New Brunswick, New Jer- sey 08933 (US). = = = Title: 6-AMINOPYRIDIN-3-YL THIAZOLES AS MODULATORS OF RORyT (54) = O R1 R 2 A 5 Il . 4 A', l'j S — NH A 4 / N (I) Il NA 1 A 2 V::+ 0\ GC 1-1 IN (57) : The present invention comprises compounds of Formula (I) wherein: A 1 , A, A 2 3 , A 4 , A, R 5 1 , and R 2 are defined in Il © the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the ei syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORyt activity P1 in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.